Formulation and investigation of 5-FU nanoparticles with factorial design-based studies


BOZKIR A., SAKA O. M.

Farmaco, cilt.60, sa.10, ss.840-846, 2005 (Scopus) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 60 Sayı: 10
  • Basım Tarihi: 2005
  • Doi Numarası: 10.1016/j.farmac.2005.06.016
  • Dergi Adı: Farmaco
  • Derginin Tarandığı İndeksler: Scopus
  • Sayfa Sayıları: ss.840-846
  • Anahtar Kelimeler: 5-Fluorouracil, Biodegradable nanoparticles, In vitro distribution, Nanoprecipitation technique, Poly(lactide-co-glycolide)
  • Ankara Üniversitesi Adresli: Evet

Özet

This study describes an orthogonal experimental design to optimize the formulation of 5-fluorouracil (5-FU) loaded poly d,l (lactide-co-glycolide) (PLGA) nanoparticles (5FU-NP) by a nanoprecipitation-solvent displacement technique. The type of surfactant, amount of acetone and molecular weight of the polymer with three levels of each factor were selected and arranged in an L18(35) orthogonal experimental table. From the statistical analysis of the data polynominal equations were generated. Optimized formulations have the particle size ranging from 160 to 250nm. Smallest nanoparticles (161 ± 1.22nm) were obtained using Resomer PLGA 755 and pluronic F-68 with 10ml acetone amount. Under these conditions the 5-FU entrapment percentage was maximum 78.30%, suggesting 5-FU might be entrapped and adsorbed on the nanoparticle surface. In vitro release of three formulations with maximum drug entrapment efficiency and minimum particle size, were also investigated by release kinetics. According to the determined coefficients, release data fit to Higuchi's diffusion kinetics. The in vitro release of 5FU-NP in phosphate buffered saline (PBS, pH 7.4) is suggested to be controlled by a combination of diffusion with slow and gradual erosion of the particles. Also, the antimicrobial activity was observed even on the end of seventh day with all formulations. © 2005 Elsevier SAS. All rights reserved.